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Published on: October 17, 2025

Farnesyl transferase inhibitors in myeloid disorders

Jeffrey E Lancet1, Judith E Karp

  • 1H. Lee Moffitt Cancer Center & Research Institute, University of South Florida, Tampa, Florida 33612, USA.

Oncology (Williston Park, N.Y.)
|September 1, 2005
PubMed

Insights

Farnesyl transferase inhibitors (FTIs) show promise as anticancer agents for myeloid malignancies. Clinical trials demonstrate target inhibition, low toxicity, and anticancer activity, with ongoing studies to optimize their therapeutic role.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Farnesyl transferase inhibitors (FTIs) are a novel class of anticancer agents.
  • Myeloid malignancies are potential targets due to overexpression of Ras, MAPK, and AKT pathways.
  • FTIs competitively inhibit farnesyl protein transferase.

Purpose of the Study:

  • To evaluate the efficacy and safety of FTIs in myeloid malignancies.
  • To assess response rates and identify downstream signaling targets of FTIs.
  • To optimize the role of FTIs in current therapeutic strategies for myeloid disorders.

Main Methods:

  • Phase I and II clinical trials were conducted.
  • Enzyme target inhibition and toxicity were assessed.
  • Downstream signal transduction targets are being identified.

Main Results:

  • Phase I trials demonstrated enzyme target inhibition, low toxicity, and anticancer activity.
  • Ongoing Phase II trials aim to assess response rates.
  • Identification of modified downstream targets is in progress.

Conclusions:

  • FTIs exhibit promising anticancer activity and favorable toxicity profiles in myeloid malignancies.
  • Further research will identify predictive biomarkers and optimal combination strategies.
  • FTIs are expected to be incorporated into therapeutic strategies for myeloid disorders.

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